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Chemical Compound Review

AGN-PC-00HPQN     17-ethynyl-13-methyl- 7,8,9,11,12,14,15,16...

Synonyms: NSC-104490, Oprea1_775480, NSC104490, AR-1C1048, AKOS001606809, ...
 
 
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Disease relevance of ethinyl estradiol

  • Significant falls in the plasma EE concentration were seen in two women (from 104.8 +/- 13.4 to 37.7 +/- 2.0 pg/ml and from 125.6 +/- 23.8 to 34.8 +/- 6.7 pg/ml p less than 0.01) and breakthrough bleeding was seen in both women [1].
 

High impact information on ethinyl estradiol

  • Despite this fact, D administration prevented some cholestatic effects of E, probably through different metabolic effects and/or direct membrane effects, not related to increased lipid lamellae excretion [2].
  • D-feeding did not prevent E-induced decrease of basal bile flow, bile salt, cholesterol, and phospholipid secretory rates nor the decrease of Na+,K+-ATPase activity and Na+-taurocholate cotransporting polypeptide (Ntcp) content in isolated sinusoidal membranes [2].
  • The kinactivation is approximately 50-fold greater than estimated for EE and is one of the highest reported for P-450 mechanism-based inactivators [3].
  • Decreased lengths of the left oviduct and its infundibulum were seen after embryonic treatment with o,p'-DDT or EE2 [4].

References

  1. The interaction of phenobarbital and other anticonvulsants with oral contraceptive steroid therapy. Back, D.J., Bates, M., Bowden, A., Breckenridge, A.M., Hall, M.J., Jones, H., MacIver, M., Orme, M., Perucca, E., Richens, A., Rowe, P.H., Smith, E. Contraception. (1980) [Pubmed]
  2. Effects of diosgenin, a plant-derived steroid, on bile secretion and hepatocellular cholestasis induced by estrogens in the rat. Accatino, L., Pizarro, M., Solís, N., Koenig, C.S. Hepatology (1998) [Pubmed]
  3. Mechanism-based inactivation of human liver microsomal cytochrome P-450 IIIA4 by gestodene. Guengerich, F.P. Chem. Res. Toxicol. (1990) [Pubmed]
  4. Embryonic exposure to o,p'-DDT causes eggshell thinning and altered shell gland carbonic anhydrase expression in the domestic hen. Holm, L., Blomqvist, A., Brandt, I., Brunstr??m, B., Ridderstr??le, Y., Berg, C. Environ. Toxicol. Chem. (2006) [Pubmed]
 
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